新型口服降糖药——二肽基肽酶-Ⅳ抑制剂

Dipeptidyl peptidase Ⅳ inhibitors:a new class of oral agents for treatment of type 2 diabetes mellitus

胰高血糖素样肽(GLP-1)在调节血糖方面起着重要的作用,但其在体内可迅速被二肽基肽酶-Ⅳ(DPP-Ⅳ)降解失活。DPP-Ⅳ抑制剂可有效抑制GLP-1的降解,通过促进胰岛素分泌、抑制胰高血糖素释放、抑制食欲、减慢胃排空等作用调节血糖,具有不易引起严重低血糖事件、不引起体重增加等特点。本文对GLP-1和DPP-Ⅳ抑制剂的作用特点及已上市使用的西格列汀、维格列汀和沙格列汀的临床疗效、药代动力学以及不良反应等方面进行了综述。

Glucagon-like peptide-1（GLP-1）, one kind of incretins, contributes to control blood glucose level with several routines. It can be degraded rapidly by the enzyme dipeptidyl peptidase Ⅳ （DPP-Ⅳ）. DPP-Ⅳ inhibitors augment glucose homeostasis by preventing degradation of GLP-1, which can stimulate insulin secretion, inhibit glucagon secretion, increase satiety, and slow gastric emptying . They are weight neutral, and are associated with low risk of hypoglycemia . This review highlights the characteristics of GLP-1, clinical efficacy, pharmacokinetics and adverse reactions of DPP-Ⅳ inhibitors.